The initial clinical study results for APD668, an oral drug candidate discovered by Arena Pharmaceuticals, Inc. suggest that glucose dependent insulinotropic receptors, or GDIRs, may improve glucose control in patients with type 2 diabetes.
APD668 was being investigated for the treatment of type 2 diabetes under a partnership with Ortho-McNeil Pharmaceutical, Inc. Based on the data from the studies, Ortho-McNeil has decided to put APD668 on hold and has advanced a potentially more potent Arena discovered GDIR agonist into preclinical development.
Ortho-McNeil's initial clinical studies evaluated healthy volunteers and patients with type 2 diabetes in randomised, double-blind, placebo-controlled trials evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple (14 day) escalating doses of APD668.
"We are encouraged by the clinical study results supporting GDIR agonists as effective modulators of glucose homeostasis in patients with type 2 diabetes, and we look forward to the results of Ortho-McNeil advancing another of Arena's GDIR compounds into development," stated Dominic P. Behan, Ph.D., senior vice president and chief scientific officer, Arena.
The GDIR is an orphan G protein-coupled receptor, or GPCR, discovered by Arena. It is expressed in beta cells, the cells in the pancreas responsible for producing insulin in response to increases in blood glucose. Stimulation of the GDIR is intended to more efficiently promote insulin release by beta cells in response to elevated blood glucose levels. In addition, in preclinical studies, the GDIR stimulates the release of GLP and GIP, two incretins that are important for proper insulin regulation, which may enhance glucose homeostasis. GDIR stimulation has also been found to increase the levels and activity of intracellular factors thought to be involved in the preservation of beta cells. The GDIR is amenable to small molecule, orally active, drug development.
Arena is a clinical-stage biopharmaceutical company focused on discovering, developing and commercialising oral drugs in four major therapeutic areas: cardiovascular, central nervous system, inflammatory and metabolic diseases.